Pharmacokinetics and pharmacodynamics of danofloxacin in serum and tissue fluids of goats following intravenous and intramuscular administration

Aliabadi, F. Shojaee; Lees, P.

doi:10.2460/ajvr.2001.62.1979

Cited by 102 publications

(125 citation statements)

References 22 publications

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“…This V ss is lower than those determined for danofloxacin in rabbits (V ss = 3.16 l kg The terminal half-life (t 1 /2λz ) after IV dosing was 15.40 h; this value was longer than those reported for florfenicol (Stamper et al 2003) and ticarcillin (Manire et al 2005) in loggerhead turtles, showing advantages, in principle, over these 2 drugs. The mean t 1 /2λz value following IM administration was 14.70 h. The fact that half-life value after IV dosing is longer than that after IM dosing has also been reported for danofloxacin and other fluoroquinolones in goats (Aliabadi & Lees 2001), sheep (Aliabadi et al 2003a) and horses (Fernández-Varón et al 2006). Therefore absorption processes do not appear to affect elimination of danofloxacin.…”

Section: Discussionmentioning

confidence: 56%

Pharmacokinetics of danofloxacin after single dose intravenous, intramuscular and subcutaneous administration to loggerhead turtles Caretta caretta

Marı́n¹,

Bayón²,

Fernández-Varón³

et al. 2008

Dis. Aquat. Org.

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Section: Discussionmentioning

confidence: 56%

Pharmacokinetics of danofloxacin after single dose intravenous, intramuscular and subcutaneous administration to loggerhead turtles Caretta caretta

Marı́n¹,

Bayón²,

Fernández-Varón³

et al. 2008

Dis. Aquat. Org.

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“…In these investigations, E max represents the baseline bacterial count and E 0 is the maximal effect of the drug inhibiting bacterial growth (1,2,5). Hence, the antibacterial response is the dependent variable representing the reduction in the initial bacterial count.…”

Section: Methodsmentioning

confidence: 99%

“…The antibacterial efficacy was quantified from the sigmoid E max equation (equation 2) by determining the C 24h /serum inhibitory activity ratios required for a bacteriostatic effect (no change in bacterial count after 24 h of incubation), a 50% reduction in the bacterial count, a bactericidal effect (a 99.9% decrease in the bacterial count), and bacterial elimination (the lowest C 24h /serum inhibitory activity ratio that produced a reduction in bacterial counts to 10 CFU/ml) in serum (1).…”

Section: Methodsmentioning

confidence: 99%

“…Increasing evidence suggests that the main PK-PD surrogate markers for fluoroquinolones correlating with clinical cure and bacterial eradication are the area under the serum concentration-time curve (AUC)/MIC ratio and the maximum concentration of the drug in serum (C max )/MIC ratio (9,46). Hence, this approach determines ex vivo PK-PD indices, which subsequently allow a more targeted design in confirmatory in vivo studies (1,2,3). PK-PD experiments with marbofloxacin were previously conducted with calves, cows, goats, and dogs (2,43,48,55).…”

mentioning

confidence: 99%

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Integration of Pharmacokinetic and Pharmacodynamic Indices of Marbofloxacin in Turkeys

Milanova

Rusenova

Parvanov

et al. 2006

Antimicrob Agents Chemother

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Fluoroquinolones are extensively used in the treatment of systemic bacterial infections in poultry, including systemic Escherichia coli bacillosis, which is a common disease in turkey flocks. Marbofloxacin has been licensed for use in various mammalian species, but not as yet for turkeys, although its kinetic properties distinguish it from other fluoroquinolones. For example, the longer half-life of marbofloxacin in many animal species has been appreciated in veterinary practice. It is generally accepted that, for fluoroquinolones, the optimal dose should be estimated on the basis of the pharmacokinetic (PK) and pharmacodynamic (PD) characteristics of the drug under consideration. Knowledge of these specific data for the target animal species allows the establishment of an integrated PK-PD model that is of high predictive value. In the present study, the antibacterial efficacy (PD indices) against a field isolate of Escherichia coli O78/K80 was investigated ex vivo following oral and intravenous administration of marbofloxacin to turkeys (breed BUT 9; six animals per group) at a dose of 2 mg/kg of body weight (BW). At the same time, the serum concentrations of marbofloxacin were measured at different time intervals by a standardized high-performance liquid chromatography method, allowing the calculation of the most relevant kinetic parameters (PK parameters). The in vitro serum inhibitory activity of marbofloxacin against the selected E. coli strain, O78/K80, was 0.5 g/ml in the blood serum of turkeys, and the ratio of the maximum concentration of the drug in serum to the serum inhibitory activity was 1.34. The lowest ratio of the measured serum concentration multiplied by the incubation period of 24 h to the serum inhibitory activity required for bacterial elimination was lower than the ratio of the area under the serum concentration-time curve (AUC) to the serum inhibitory activity. These first results suggested that the recommended dose of 2 mg/kg BW of marbofloxacin is sufficient to achieve a therapeutic effect in diseased animals. However, considering the risk of resistance induction, the applied dose should be equal to an AUC/MIC of >125, the generally recommended dose for all fluoroquinolones. According to the PK-PD results presented here, a dose of 3.0 to 12.0 mg/kg BW per day would be needed to meet this criterion. In conclusion, the results of the present study provide the rationale for an optimal dose regimen for marbofloxacin in turkeys and hence should form the basis for dose selection in forthcoming clinical trials.Marbofloxacin is a synthetic fluoroquinolone, developed for veterinary use only (47). It has a broad spectrum of activity (58), and bactericidal concentration-dependent killing is observed against many gram-negative bacteria (12, 49, 51, 52). The pharmacokinetic (PK) properties of marbofloxacin have been studied in several mammalian species, and some advantages over other fluoroquinolones, such as a longer elimination half-life, have been described (2,43,47,48). In practice, this would e...

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“…GAT has a chiral center in its structure, exists in plasma as two equi-active equi-proportional R-and S-enantiomers (Wise et al, 1999). Fluoroquinolones act by a concentration-dependent killing mechanism (Drusano et al, 1993), which is associated with a relatively prolonged postantibiotic effect (Aliabadi and Lees, 2001). …”

Section: Introductionmentioning

confidence: 99%

Effect of Induced Mastitis on Disposition Kinetics of Gatifloxacin Following Intravenous Administration in Goats

Ram¹,

Roy²,

Singh³

2010

JBABM

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Pharmacokinetics and pharmacodynamics of danofloxacin in serum and tissue fluids of goats following intravenous and intramuscular administration

Abstract: Integration of danofloxacin pharmacokinetic and pharmacodynamic data obtained in goats may provide a new approach on which to base recommendations for therapeutic dosages.

Cited by 102 publications

References 22 publications

Pharmacokinetics of danofloxacin after single dose intravenous, intramuscular and subcutaneous administration to loggerhead turtles Caretta caretta

Pharmacokinetics of danofloxacin after single dose intravenous, intramuscular and subcutaneous administration to loggerhead turtles Caretta caretta

Integration of Pharmacokinetic and Pharmacodynamic Indices of Marbofloxacin in Turkeys

Effect of Induced Mastitis on Disposition Kinetics of Gatifloxacin Following Intravenous Administration in Goats

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